Meropenem powder for injection 500mg bottle №1

Farmgroup: antibiotic-carbapenem.

Pharmaceutical action:

An antibiotic from the group of carbapenems for parenteral use. Resistant to dehydropeptidase-1, bactericidal (suppresses the synthesis of the bacterial cell wall), easily penetrates the bacterial cell wall, resistant to most beta-lactamase, has a high affinity for penicillin-binding proteins (PBPs).
Among the known beta-lactam antibiotics, it has the highest activity against most aerobic and anaerobic gram-positive and gram-negative microorganisms. It interacts with receptors - specific penicillin-binding proteins on the surface of the cytoplasmic membrane, inhibits the synthesis of the peptidoglycan cell wall layer (due to structural similarities), inhibits transpeptidase, promotes the release of autolytic cell wall enzymes, which ultimately causes its damage and the death of bacteria.

When intravenous injection of 250 mg for 30 minutes Cmax - 11 mcg / ml, for a dose of 500 mg - 23 mcg / ml, 1 g - 49 mcg / ml (there is no absolute pharmacokinetic proportional dependence on the administered dose for Cmax and AUC). When increasing the dose from 250 mg to 2 g, the clearance decreases from 287 to 205 ml / min. For intravenous bolus administration for 5 minutes, 500 mg Cmax - 52 mcg / ml, 1 g - 112 mcg / ml.
Communication with plasma proteins - 2%. It penetrates well into most tissues and body fluids, incl. in CSF of patients with bacterial meningitis, reaching concentrations exceeding those required for suppressing most bacteria (bactericidal concentrations are created 0.5–1.5 h after the start of the infusion). In small quantities penetrates into breast milk.
Subjected to minor metabolism in the liver with the formation of a single inactive metabolite. T1 / 2 - 1 h, in children up to 2 years old - 1.5-2.3 h. In the dose range of 10-40 mg / kg in adults and children, a linear dependence of pharmacokinetic parameters is observed. Does not accumulate.
Excreted by the kidneys - 70% unchanged for 12 hours. The concentration of meropenem in the urine, exceeding 10 mcg / ml, is maintained for 5 hours after the administration of 500 mg. In patients with renal insufficiency, clearance correlates with CC. In elderly patients, a decrease in clearance of meropenem correlates with a decrease in CC due to age. T1 / 2-1.5 hours. It is displayed during hemodialysis.

Indications and usage

Bacterial infections caused by susceptible pathogens (as monotherapy or combination with other antiviral and antifungal drugs): infections of the lower respiratory tract (including pneumonia, including nosocomial infections; infections caused by Pseudomonas bacilli), abdominal infections (complicated appendicitis, peritonitis, pelvioperitonitis), pyelonephritis, pyelitis, infections of the skin and soft tissues (including erysipelas, impetigo, secondarily infected dermatosis), dysentery, endocarditis,bacterial meningitis, sepsis, inflammatory diseases of the pelvic organs (including endometritis), suspected bacterial infection in adults with febrile episodes against neutropenia (empirical treatment).

Contraindications

Hypersensitivity, pregnancy, lactation, child age (under 3 months).

Special notes

Patients with a history of hypersensitivity to carbapenems, penicillins or other beta-lactam antibiotics may be hypersensitive to meropenem.
Treatment of patients with liver diseases should be carried out under the careful control of the activity of liver transaminases and bilirubin concentrations.
In the course of treatment, the development of pathogen resistance is possible, and therefore long-term treatment is carried out under the constant control of the spread of resistant strains.
In individuals with complaints of the gastrointestinal tract, especially those suffering from colitis, it is necessary to take into account the possibility of developing pseudomembranous colitis (the toxin produced by Clostridium difficile is one of the main causes of antibiotic-related colitis), the first symptom of which may be diarrhea during treatment.
When monotherapy is known or suspected infection of the lower respiratory tract severe, caused by Pseudomonas aeruginosa, it is recommended to regularly determine the sensitivity of the pathogen.
During pregnancy and lactation, it is necessary to evaluate the potential advantage and the possible risk from the use of the drug for the fetus, infant and mother.

Dosage and administration

B / bolus (diluted with sterile water, 5 ml per 250 mg), for 5 minutes or by infusion, for 15-30 minutes (to 50-200 ml with a compatible infusion fluid).
Adults with pneumonia, urinary tract infections, gynecological infections and pelvic inflammatory diseases, infections of the skin and soft tissues - in / in, 500 mg every 8 hours;
with hospital pneumonia, peritonitis, sepsis, suspected bacterial infection in patients with neutropenia - in / in, 1 g 3 times a day;
for meningitis, 2 g every 8 h.
In case of chronic kidney disease, the dose is adjusted depending on CC: with CC 26-50 ml / min - 0.5-1 g 2 times a day, 10-25 ml / min - 250-500 mg 2 times a day, less than 10 ml / min - 500 mg 1 time per day.
Children aged 3 months. up to 12 years a single dose for IV - 10-20 mg / kg 3 times a day; for children weighing more than 50 kg, dosages for adults are used; meningitis - in / in, 40 mg / kg every 8 hours.
Experience with children with impaired renal function is absent.

Adverse reactions

On the part of the digestive system: pain in the epigastric region, nausea, vomiting, diarrhea, cholestatic hepatitis, hyperbilirubinemia, increased activity of “liver” transaminases and alkaline phosphatase, LDH, rarely - oral candidiasis, pseudomembranous enterocolitis.
On the part of the cardiovascular system: the development or worsening of heart failure, cardiac arrest, tachy- or bradycardia, decrease or increase in blood pressure, fainting, myocardial infarction, thromboembolism of the branches of the pulmonary artery.
On the part of the urinary system: dysuria, edema, impaired renal function (hypercreatininemia, increased concentration of urea in the plasma), hematuria. Allergic reactions: skin itching, skin rash, urticaria, erythema multiforme exudative, angioedema, anaphylactic shock.
Nervous system disorders: headache, paresthesias, insomnia, irritability, anxiety, depression, impaired consciousness, hallucinations, epileptiform seizures, convulsions.
On the part of laboratory parameters: eosinophilia, neutropenia, leukopenia, rarely - agranulocytosis, reversible thrombocytopenia, reduced partial thromboplastin time.
Local reactions: inflammation, thrombophlebitis, pain at the injection site; tissue damage with a concomitant rise in CPK (for intramuscular injection).
Other: positive direct or indirect Coombs test, anemia, dyspnea, vaginal candidiasis.

Drug Interactions

Incompatible with Heparin.
Compatible with 0.9% NaCl solution, 5% or 10% dextrose solution, with 0.02% sodium bicarbonate solution, 5% dextrose solution with 0.225% NaCl, 5% dextrose solution with 0.15% KC1, 2.5% and 10% mannitol solution.
Ganciclovir increases the risk of developing generalized seizures.
Shows antagonism when interacting with beta-lactam antibiotics.
Drugs blocking tubular secretion, slow down the excretion and increase the concentration in plasma.